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New antifungal 1,2,4-triazoles with difluoro(substituted sulfonyl)methyl moiety
1Central Research Labs., SS Pharmaceutical Co., Ltd., Narita, Chiba, Japan. Hiromichi.Eto@ssp.co.jp
Chemical & Pharmaceutical Bulletin
|February 24, 2001
Abstract:
New 1,2,4-triazoles (2) having a difluoro(substituted sulfonyl)methyl moiety were designed and synthesized via alpha,alpha-difluoro-alpha-(substituted thio)acetophenones (3). Compounds (2) showed potent antifungal activities against C. albicans, C. krusei, A. flavus and A. fumigatus in vitro and against C. albicans in vivo for oral and i.v. administrations. Especially, (-)-2a, (-)-2b and (-)-2d showed potent antifungal activities.